Cancer is a major health problem worldwide. Particularly, lung cancer is the leading cause of cancer deaths worldwide. Non-small cell lung cancer (NSCLC) accounts for about 80% of all lung cancers. Despite the recent advantages of therapies, the disease is rarely curable, with poor prognosis and overall 5-year survival rate of only 15%. With current platinum-based chemotherapy regimens, medial survival is 7-10 months. Progress in understanding of the cancer biology and mechanisms of oncogenesis has allowed the development of several potential molecular targets for NSCLC treatment. Several targeted agents have been introduced in clinical trials in NSCLC. The main agents that have been investigated are epidermal growth factor receptor (EGFR), tyrosine kinase family inhibitors (TKIs), angiogenesis inhibitors, and various signal transduction inhibitors. EGFR-TKIs, such as gefitinib and erlotinib, are active as single agents only in small subsets of patients with specific biological and/or pathological features. There exists an unmet need for agents suitable for treating cancers, particularly heterogeneous cancers such as lung cancer.